EP2331501A4 - Small molecule inhibitors of n-terminus activation of the androgen receptor - Google Patents
Small molecule inhibitors of n-terminus activation of the androgen receptorInfo
- Publication number
- EP2331501A4 EP2331501A4 EP20090807798 EP09807798A EP2331501A4 EP 2331501 A4 EP2331501 A4 EP 2331501A4 EP 20090807798 EP20090807798 EP 20090807798 EP 09807798 A EP09807798 A EP 09807798A EP 2331501 A4 EP2331501 A4 EP 2331501A4
- Authority
- EP
- European Patent Office
- Prior art keywords
- small molecule
- androgen receptor
- molecule inhibitors
- terminus
- activation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 230000004913 activation Effects 0.000 title 1
- 102000001307 androgen receptors Human genes 0.000 title 1
- 108010080146 androgen receptors Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003384 small molecules Chemical class 0.000 title 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/38—2-Pyrrolones
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Ophthalmology & Optometry (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13627708P | 2008-08-22 | 2008-08-22 | |
PCT/CA2009/001173 WO2010020055A1 (en) | 2008-08-22 | 2009-08-24 | Small molecule inhibitors of n-terminus activation of the androgen receptor |
Publications (3)
Publication Number | Publication Date |
---|---|
EP2331501A1 EP2331501A1 (en) | 2011-06-15 |
EP2331501A4 true EP2331501A4 (en) | 2012-06-06 |
EP2331501B1 EP2331501B1 (en) | 2016-07-20 |
Family
ID=41706796
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP09807798.5A Active EP2331501B1 (en) | 2008-08-22 | 2009-08-24 | Small molecule inhibitors of n-terminus activation of the androgen receptor |
Country Status (14)
Country | Link |
---|---|
US (2) | US9487479B2 (en) |
EP (1) | EP2331501B1 (en) |
JP (1) | JP2012500778A (en) |
CN (1) | CN102131775B (en) |
AU (1) | AU2009284668B2 (en) |
BR (1) | BRPI0917818A2 (en) |
CA (1) | CA2728103C (en) |
CL (1) | CL2011000341A1 (en) |
CO (1) | CO6351779A2 (en) |
ES (1) | ES2593859T3 (en) |
HK (1) | HK1153198A1 (en) |
MX (1) | MX339300B (en) |
RU (1) | RU2519948C2 (en) |
WO (1) | WO2010020055A1 (en) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2012500778A (en) | 2008-08-22 | 2012-01-12 | ブリティッシュ コロンビア キャンサー エージェンシー ブランチ | Small molecule inhibitors of N-terminal activation of androgen receptor |
NZ726348A (en) | 2014-05-30 | 2022-09-30 | Univ British Columbia | Androgen receptor modulators and methods for their use |
TWI726969B (en) | 2016-01-11 | 2021-05-11 | 比利時商健生藥品公司 | Substituted thiohydantoin derivatives as androgen receptor antagonists |
US10799416B2 (en) * | 2017-01-11 | 2020-10-13 | Jonathan Taves | Self-treating upper neck system for therapeutic mobilization |
CN107353239B (en) | 2017-08-11 | 2019-06-18 | 北京卓凯生物技术有限公司 | 4- oxygen-alkylation tetramates acids compound and preparation method thereof |
CN107468690B (en) * | 2017-08-11 | 2020-01-31 | 北京卓凯生物技术有限公司 | 4-oxygen-alkylated tetramic acid compound and preparation method and application thereof |
RU2700573C2 (en) * | 2017-10-16 | 2019-09-18 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Кировский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО Кировский ГМУ Минздрава России) | Method of castration-resistant prostate cancer treatment |
RU2694259C2 (en) * | 2017-10-16 | 2019-07-11 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Кировский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО Кировский ГМУ Минздрава России) | Method of castration-resistant prostate cancer treatment |
RU2696287C2 (en) * | 2017-10-16 | 2019-08-01 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Кировский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО Кировский ГМУ Минздрава России) | Method of castration-resistant prostate cancer treatment |
RU2694373C2 (en) * | 2017-10-16 | 2019-07-12 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Кировский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО Кировский ГМУ Минздрава России) | Method of castration-resistant prostate cancer treatment |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0317057A (en) * | 1989-06-15 | 1991-01-25 | Fujisawa Pharmaceut Co Ltd | New 5-membered ring heterocyclic compound |
AU4494399A (en) | 1998-06-30 | 2000-01-24 | University Of British Columbia, The | Inhibitors of androgen-independent activation of androgen receptor |
EP1282609B1 (en) * | 2000-05-09 | 2008-12-17 | AngioRx Corporation | Piperazinedione compounds |
GB0130677D0 (en) * | 2001-12-21 | 2002-02-06 | Glaxo Group Ltd | Medicaments and novel compounds |
US7772433B2 (en) | 2002-02-28 | 2010-08-10 | University Of Tennessee Research Foundation | SARMS and method of use thereof |
JP2012500778A (en) | 2008-08-22 | 2012-01-12 | ブリティッシュ コロンビア キャンサー エージェンシー ブランチ | Small molecule inhibitors of N-terminal activation of androgen receptor |
NZ726348A (en) | 2014-05-30 | 2022-09-30 | Univ British Columbia | Androgen receptor modulators and methods for their use |
-
2009
- 2009-08-24 JP JP2011523280A patent/JP2012500778A/en not_active Abandoned
- 2009-08-24 CN CN200980132751.6A patent/CN102131775B/en active Active
- 2009-08-24 US US12/999,035 patent/US9487479B2/en active Active
- 2009-08-24 MX MX2011001890A patent/MX339300B/en active IP Right Grant
- 2009-08-24 AU AU2009284668A patent/AU2009284668B2/en active Active
- 2009-08-24 EP EP09807798.5A patent/EP2331501B1/en active Active
- 2009-08-24 RU RU2011110743/04A patent/RU2519948C2/en active
- 2009-08-24 WO PCT/CA2009/001173 patent/WO2010020055A1/en active Application Filing
- 2009-08-24 ES ES09807798.5T patent/ES2593859T3/en active Active
- 2009-08-24 CA CA2728103A patent/CA2728103C/en active Active
- 2009-08-24 BR BRPI0917818A patent/BRPI0917818A2/en not_active IP Right Cessation
-
2011
- 2011-02-17 CL CL2011000341A patent/CL2011000341A1/en unknown
- 2011-03-22 CO CO11034471A patent/CO6351779A2/en not_active Application Discontinuation
- 2011-07-18 HK HK11107462.1A patent/HK1153198A1/en unknown
-
2016
- 2016-09-27 US US15/277,733 patent/US20170239216A1/en not_active Abandoned
Non-Patent Citations (4)
Title |
---|
HOSSEINI MASOOD ET AL: "Dipeptide Analogues Containing 4-Ethoxy-3-pyrrolin-2-ones", ORGANIC LETTERS, AMERICAN CHEMICAL SOCIETY, US, vol. 8, no. 10, 11 May 2006 (2006-05-11), pages 2103 - 2106, XP009155629, ISSN: 1523-7060 * |
HOSSEINI MASOOD ET AL: "Pyrrolidinone-modified di- and tripeptides: Highly diastereoselective preparation and investigation of their stability", ORGANIC & BIOMOLECULAR CHEMISTRY, ROYAL SOCIETY OF CHEMISTRY, GB, vol. 5, no. 21, 1 January 2007 (2007-01-01), pages 3486 - 3494, XP009155628, ISSN: 1477-0520 * |
LUESCH H ET AL: "Structurally diverse new alkaloids from Palauan collections of the apratoxin-producing marine cyanobacterium Lyngbya sp", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 58, no. 39, 23 September 2002 (2002-09-23), pages 7959 - 7966, XP004381451, ISSN: 0040-4020, DOI: 10.1016/S0040-4020(02)00895-5 * |
See also references of WO2010020055A1 * |
Also Published As
Publication number | Publication date |
---|---|
EP2331501A1 (en) | 2011-06-15 |
EP2331501B1 (en) | 2016-07-20 |
CL2011000341A1 (en) | 2011-09-02 |
AU2009284668A1 (en) | 2010-02-25 |
AU2009284668B2 (en) | 2015-07-09 |
HK1153198A1 (en) | 2012-03-23 |
US20110230539A1 (en) | 2011-09-22 |
CA2728103C (en) | 2017-06-27 |
WO2010020055A1 (en) | 2010-02-25 |
JP2012500778A (en) | 2012-01-12 |
CN102131775B (en) | 2015-12-16 |
CO6351779A2 (en) | 2011-12-20 |
US20170239216A1 (en) | 2017-08-24 |
US9487479B2 (en) | 2016-11-08 |
BRPI0917818A2 (en) | 2017-02-21 |
MX2011001890A (en) | 2011-06-20 |
ES2593859T3 (en) | 2016-12-13 |
RU2011110743A (en) | 2012-09-27 |
CA2728103A1 (en) | 2010-02-25 |
CN102131775A (en) | 2011-07-20 |
MX339300B (en) | 2016-05-19 |
RU2519948C2 (en) | 2014-06-20 |
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